Discovery and initial SAR of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-ones as inhibitors of insulin-like growth factor 1-receptor (IGF-1R).

doi:10.1016/J.BMCL.2007.01.102

Paper

Discovery and initial SAR of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-ones as inhibitors of insulin-like growth factor 1-receptor (IGF-1R).

Published Apr 15, 2007 · Upender Velaparthi, M. Wittman, Peiying Liu

Bioorganic & medicinal chemistry letters

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36

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2

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Abstract

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Study Snapshot

3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-ones show potential as inhibitors of insulin-like growth factor 1-receptor (IGF-1R), with improved enzyme potency when amine-containing side chains are added at the 4-position of

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Discovery and initial SAR of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-ones as inhibitors of insulin-like growth factor 1-receptor (IGF-1R).

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References

The cyclolignan PPP induces activation loop-specific inhibition of tyrosine phosphorylation of the insulin-like growth factor-1 receptor. Link to the phosphatidyl inositol-3 kinase/Akt apoptotic pathway

Cyclolin PPP preferentially inhibits phosphorylated Akt in neoplastic cells by specifically inhibiting Y1136 in the insulin-like growth factor-1 receptor, without directly interfering with Akt or its downstream molecules in the apoptotic pathway.

Targeting insulin-like growth factor pathways

Targeting the type I IGF receptor (IGF-IR) shows potential for cancer therapy, but early clinical trials must address safety and efficacy issues.

Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.

BMS-536924 shows in vivo antitumor activity, with potential for use in cancer therapy.

The insulin-like growth factor-I receptor as a target for cancer therapy

Targeting the IGF-I receptor in cancer therapy may cause tumor cell apoptosis and resistance to viral and cellular oncogenes, potentially leading to a cure for human tumors.

Blocking the insulin-like growth factor-I receptor as a strategy for targeting cancer.

Blocking the insulin-like growth factor-I receptor may be a promising strategy for treating cancer by targeting its signaling pathway.

Citations